143 articles for Y Lu
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Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRa) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs).
East China University of Science and Technology
Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis.
Peking Union Medical College
Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer.
University of Illinois College of Pharmacy
Gossypol with Hydrophobic Linear Esters Exhibits Enhanced Antitumor Activity as an Inhibitor of Antiapoptotic Proteins.
Wuhan University School of Pharmaceutical Sciences
Discovery of Benzocycloalkane Derivatives Efficiently Blocking Bacterial Virulence for the Treatment of Methicillin-Resistant S. aureus (MRSA) Infections by Targeting Diapophytoene Desaturase (CrtN).
East China University of Science and Technology
Discovery of Potent Benzofuran-Derived Diapophytoene Desaturase (CrtN) Inhibitors with Enhanced Oral Bioavailability for the Treatment of Methicillin-Resistant Staphylococcus aureus (MRSA) Infections.
East China University of Science and Technology
Development of CINPA1 analogs as novel and potent inverse agonists of constitutive androstane receptor.
St. Jude Children'S Research Hospital
Polyketides witha-Glucosidase Inhibitory Activity from a Mangrove Endophytic Fungus, Penicillium sp. HN29-3B1.
Hebei University
Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.
Novartis Institutes For Biomedical Research
Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors.
Novartis Institutes For Biomedical Research
Synthesis of Deuterated Benzopyran Derivatives as Selective COX-2 Inhibitors with Improved Pharmacokinetic Properties.
Institutes of Biomedicine and Health
Radiosynthesis and biological evaluation of a novel enoyl-ACP reductase inhibitor for Staphylococcus aureus.
Stony Brook University
Evaluation of aminohydantoins as a novel class of antimalarial agents.
Saint Louis University
Discovery and synthesis of novel 4-aminopyrrolopyrimidine Tie-2 kinase inhibitors for the treatment of solid tumors.
Pfizer
Antidepressant abietane diterpenoids from Chinese eaglewood.
Peking Union Medical College
The effect of absolute configuration on activity, subtype selectivity (M3/M2) of 3a-acyloxy-6ß-acetoxyltropane derivatives as muscarinic M3 receptor antagonists.
Shanghai Jiao Tong University
Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.
TBA
Azaphilones and p-terphenyls from the mangrove endophytic fungus Penicillium chermesinum (ZH4-E2) isolated from the South China Sea.
Sun Yat-Sen University
"Carba"-analogues of fentanyl are opioid receptor agonists.
Clinical Research Institute of Montreal
Benzylphenethylamine alkaloids from Hosta plantaginea with inhibitory activity against tobacco mosaic virus and acetylcholinesterase.
Chinese Academy of Sciences
Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation.
Pfizer
[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
Clinical Research Institute of Montreal
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Research Triangle Institute
Discovery of Lu AA33810: a highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder.
Lundbeck Research Usa
Synthesis and pharmacological evaluation of the stereoisomers of 3-carba cyclic-phosphatidic acid.
University of Tennessee Health Science Center
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.
Novartis Institutes For Biomedical Research
2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors.
Ligand Pharmaceuticals
Synthesis, in vitro structure-activity relationship, and in vivo studies of 2-arylthiazolidine-4-carboxylic acid amides as anticancer agents.
University of Tennessee Health Science Center
Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.
Philipps University Marburg
A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties.
Sunesis Pharmaceuticals
Halogen bonding--a novel interaction for rational drug design?
Chinese Academy of Sciences
Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047).
Proteolix
Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio.
Sunesis Pharmaceuticals
Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].
National University of Singapore
Synthesis, cytotoxicity, antioxidant activity and molecular modeling of new NSAIDs-EBS derivatives.
Jianghan University
Discovery of a novel dual-target inhibitor of CDK12 and PARP1 that induces synthetic lethality for treatment of triple-negative breast cancer.
Southwest Jiaotong University
Highly-tumor-targeted PAD4 inhibitors with PBA modification inhibit tumors in vivo by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils.
College of Pharmaceutical Sciences of Capital Medical University
Design, synthesis and biological evaluation of 3-substituted-2-thioxothiazolidin-4-one (rhodanine) derivatives as antitubercular agents against Mycobacterium tuberculosis protein tyrosine phosphatase B.
Peking Union Medical College and Chinese Academy of Medical Sciences
Structure-affinity relationships of stereoisomers of norbenzomorphan-derived σ2R/TMEM97 modulators.
The University of Texas at Austin
Discovery of 3-oxo-1,2,3,4-tetrahydropyrido[1,2-a]pyrazin derivatives as SARS-CoV-2 main protease inhibitors through virtual screening and biological evaluation.
Peking University
Discovery of Novel Heterotricyclic Compounds as DNA-Dependent Protein Kinase (DNA-PK) Inhibitors with Enhanced Chemosensitivity, Oral Bioavailability, and the Ability to Potentiate Cancer Immunotherapy.
The Sixth Affiliated Hospital of Wenzhou Medical University
Discovery of N-(1-(6-Oxo-1,6-dihydropyrimidine)-pyrazole) Acetamide Derivatives as Novel Noncovalent DprE1 Inhibitors against Mycobacterium tuberculosis.
Zhejiang University
Recent progress and applications of small molecule inhibitors of Keap1-Nrf2 axis for neurodegenerative diseases.
Hangzhou City University
Benzothiozinone derivatives with anti-tubercular Activity-Further side chain investigation.
Suzhou Medical College of Soochow University
Cyclic Peptide Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Design, Synthesis, and In Vivo Treatment of Acute Lung Injury.
Fujian University of Traditional Chinese Medicine
Dual-targeting compounds possessing enhanced anticancer activity via microtubule disruption and histone deacetylase inhibition.
National Taiwan University
Discovery of Small and Bifunctional Molecules Targeting PD-L1/CD73 for Cancer Dual Immunotherapy.
Wenzhou Medical University Lishui Hospital
A β-Carboline Derivate PAD4 Inhibitor Reshapes Neutrophil Phenotype and Improves the Tumor Immune Microenvironment against Triple-Negative Breast Cancer.
Capital Medical University
Discovery of a Covalent Inhibitor That Overcame Resistance to Venetoclax in AML Cells Overexpressing BFL-1.
University of Chinese Academy of Sciences
Discovery of potent small molecule ubiquitin-specific protease 10 inhibitors with anti-hepatocellular carcinoma activity through regulating YAP expression.
Zhejiang University
Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.
Johnson & Johnson Pharmaceutical Research & Development
A chemical perspective on the modulation of TEAD transcriptional activities: Recent progress, challenges, and opportunities.
Shanghai Institute of Materia Medica
Discovery of Novel d-(+)-Biotin-Conjugated Resorcinol Dibenzyl Ether-Based PD-L1 Inhibitors for Targeted Cancer Immunotherapy.
Zunyi Medical University
Discovery of an Anti-TNF-α 9-mer Peptide from a T7 Phage Display Library for the Treatment of Inflammatory Bowel Disease.
Tongji University
A TNF-α blocking peptide that reduces NF-κB and MAPK activity for attenuating inflammation.
Changchun University of Science and Technology
Deciphering the multifunctional role of dual leucine zipper kinase (DLK) and its therapeutic potential in disease.
Southwest Jiaotong University
Targeting Death-Associated Protein Kinases for Treatment of Human Diseases: Recent Advances and Future Directions.
Southwest Jiaotong University
Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor.
Johnson & Johnson Pharmaceutical Research & Development
Current advances in Vibrio harveyi quorum sensing as drug discovery targets.
Zhejiang University
Selective Estrogen Receptor Degraders (SERDs): A Promising Strategy for Estrogen Receptor Positive Endocrine-Resistant Breast Cancer.
Nanjing University of Chinese Medicine
Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists.
National University of Singapore
Discovery of biphenyls bearing thiobarbiturate fragment by structure-based strategy as Mycobacterium tuberculosis protein tyrosine phosphatase B inhibitors.
Peking Union Medical College and Chinese Academy of Medical Sciences
Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis.
Peking Union Medical College and Chinese Academy of Medical Sciences
The discovery of 1, 3-diamino-7H-pyrrol[3, 2-f]quinazoline compounds as potent antimicrobial antifolates.
Peking Union Medical College
Design and modular parallel synthesis of a MCR derived alpha-helix mimetic protein-protein interaction inhibitor scaffold.
Abc Pharma
Design, synthesis and biological evaluation of nitrofuran-1,3,4-oxadiazole hybrids as new antitubercular agents.
Peking Union Medical College
Discovery of 2-(furan-2-ylmethylene)hydrazine-1-carbothioamide derivatives as novel inhibitors of SARS-CoV-2 main protease.
Peking University
1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum.
The Ohio State University
Design, Synthesis, and Biological Evaluation of Pyrrole-2-carboxamide Derivatives as Mycobacterial Membrane Protein Large 3 Inhibitors for Treating Drug-Resistant Tuberculosis.
Peking Union Medical College and Chinese Academy of Medical Sciences
Enantiomerically pure hexahydropyrazinoquinolines as potent and selective dopamine 3 subtype receptor ligands.
University of Michigan
Recent advance of peptide-based molecules and nonpeptidic small-molecules modulating PD-1/PD-L1 protein-protein interaction or targeting PD-L1 protein degradation.
Zhejiang University
Development of 6-Methanesulfonyl-8-nitrobenzothiazinone Based Antitubercular Agents.
Soochow University
A novel cyclic enkephalin analogue with potent opioid antagonist activity.
Clinical Research Institute of Montreal
N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents: Synthesis and biological evaluation.
Lanzhou University
Optimization of TopoIV Potency, ADMET Properties, and hERG Inhibition of 5-Amino-1,3-dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Identification of a Lead with
The Ohio State University
Identification of Novel Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents with Excellent Pharmacokinetic Profiles against Drug-Resistant Pathogens.
Peking Union Medical College
Design, synthesis and biological evaluation of quinazoline derivatives as potent and selective FGFR4 inhibitors.
Zhejiang University
Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities.
Peking Union Medical College and Chinese Academy of Medical Sciences
Structural and Activity Relationships of 6-Sulfonyl-8-Nitrobenzothiazinones as Antitubercular Agents.
Soochow University
Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK).
China Pharmaceutical University
Discovery of N-substituted sulfamoylbenzamide derivatives as novel inhibitors of STAT3 signaling pathway based on Niclosamide.
The First Affiliated Hospital of Wenzhou Medical University
Design, synthesis and biological evaluation of diamino substituted cyclobut-3-ene-1,2-dione derivatives for the treatment of drug-resistant tuberculosis.
Peking Union Medical College
Novel bacterial topoisomerase inhibitors derived from isomannide.
The Ohio State University
Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late I
Gilead Sciences
The optimization and characterization of functionalized sulfonamides derived from sulfaphenazole against Mycobacterium tuberculosis with reduced CYP 2C9 inhibition.
Beijing University of Technology
Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics.
Bristol-Myers Squibb
Dioxane-Linked Amide Derivatives as Novel Bacterial Topoisomerase Inhibitors against Gram-Positive
The Ohio State University
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
Peking Union Medical College and Chinese Academy of Medical Sciences
Design and synthesis of 1,3-benzothiazinone derivatives as potential anti-inflammatory agents.
Lanzhou University
Discovery of novel 1,3,5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR.
Maternal and Child Health Hospital of Hubei Province
Design, synthesis and bioactivity study of N-salicyloyl tryptamine derivatives as multifunctional agents for the treatment of neuroinflammation.
Lanzhou University
The optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119.
Chinese Academy of Medical Sciences&Peking Union Medical College
Discovery and optimization of a potent and selective indazolamine series of IRAK4 inhibitors.
Zhejiang Hisun Pharmaceutical
4-Aryl Pyrrolidines as Novel Orally Efficacious Antimalarial Agents. Part 2: 2-Aryl-
Saint Louis University
Stereospecific synthesis of (2S)-2-methyl-3-(2',6'-dimethyl-4'-hydroxyphenyl)-propionic acid (Mdp) and its incorporation into an opioid peptide.
Clinical Research Institute of Montreal
Structure-activity relationships of a series of pyrrolo[3,2-d]pyrimidine derivatives and related compounds as neuropeptide Y5 receptor antagonists.
Amgen
Thiolactomycin-Based Inhibitors of Bacterial β-Ketoacyl-ACP Synthases with in Vivo Activity.
Colorado State University
4-Aryl Pyrrolidines as a Novel Class of Orally Efficacious Antimalarial Agents. Part 1: Evaluation of 4-Aryl- N-benzylpyrrolidine-3-carboxamides.
Saint Louis University
Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones.
Peking Union Medical College
Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents.
Peking Union Medical College
Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer.
University of Illinois At Chicago
Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms.
West China Hospital of Sichuan University
Phenolic group on A-ring is key for dracoflavan B as a selective noncompetitive inhibitor of α-amylase.
National University of Singapore
Application of the bicyclo[1.1.1]pentane motif as a nonclassical phenyl ring bioisostere in the design of a potent and orally active γ-secretase inhibitor.
Pfizer
Metabolism-directed design of oxetane-containing arylsulfonamide derivatives as γ-secretase inhibitors.
Pfizer
Quantitative structure-selectivity relationship for M2 selectivity between M1 and M2 of piperidinyl piperidine derivatives as muscarinic antagonists.
Shanghai Jiao Tong University School of Medicine
Activity and QSAR study of baogongteng A and its derivatives as muscarinic agonists.
Shanghai Second Medical University
Solution phase parallel synthesis and evaluation of MAPK inhibitory activities of close structural analogues of a Ras pathway modulator.
Morphochem
Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors.
University of Illinois At Chicago
Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer.
Chinese Academy of Sciences
Pentafluorosulfanyl-Substituted Benzopyran Analogues As New Cyclooxygenase-2 Inhibitors with Excellent Pharmacokinetics and Efficacy in Blocking Inflammation.
Guangzhou Institutes of Biomedicine and Health
Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria.
Novartis Institutes For Biomedical Research
Design, Synthesis, and Properties of a Potent Inhibitor of Pseudomonas aeruginosa Deacetylase LpxC.
Novartis Institutes For Biomedical Research
Discovery of an Orally Bioavailable Inhibitor of Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation.
St. Jude Children'S Research Hospital
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
East China University of Science and Technology
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Moe) and Hubei Provinc
INHIBITORS OF ANTIMOCROBIAL RESISTANCE AND METHOS USING SAME
Baylor College of Medicine
FUSED BICYCLIC COMPOUND CONTAINING PYRROLINONE
Chia Tai Tianqing Pharmaceutical Group
2-OXO-DIHYDROQUINOLINE-3-CARBOXAMIDE DERIVATIVES AS GABA TYPE A RECEPTOR MODULATORS
University College Cardiff Consultants
USE OF SOS1 INHIBITORS TO TREAT MALIGNANCIES WITH SHP2 MUTATIONS
Revolution Medicines
Degradation of tripartite motif-containing protein 24 (TRIM24) by conjugation of TRIM24 inhibitors with E3 ligase ligand and methods of use
Dana-Farber Cancer Institute
Substituted indazole derivatives active as kinase inhibitiors
Nerviano Medical Sciences
Metabotropic glutamate receptor positive allosteric modulators (PAMS) and uses thereof
Sanford-Burnham Medical Research Institute
New IDH1 mutant inhibitors for treatment of acute myeloid leukemia
Albert Einstein College of Medicine
Development and biological evaluation of a novel aurora A kinase inhibitor.
Parc De Recerca Biomedica De Barcelona
Structure-based optimization of novel azepane derivatives as PKB inhibitors.
Roche Diagnostics
Design and crystal structures of protein kinase B-selective inhibitors in complex with protein kinase A and mutants.
Max-Planck-Institut Fuer Biochemie
The complex of a bivalent derivative of galanthamine with torpedo acetylcholinesterase displays drastic deformation of the active-site gorge: implications for structure-based drug design.
Weizmann Institute of Science
Nonpeptidal P2 ligands for HIV protease inhibitors: structure-based design, synthesis, and biological evaluation.
University of Illinois At Chicago